Activators & Inhibitors

HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated inhibitor of HDAC6 (IC50= 0.025 μM). HDAC6-IN-5 inhibits Aβ 1-42 self-aggregation and AChE, with IC 50s of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity.

pan-HER-IN-1 (Compound C5) is an irreversible, orally active pan- HER inhibitor. pan-HER-IN-1 exhibits IC 50s of 0.38, 1.6, 2.2 and 3.5 nM for EGFR, HER4, EGFR T790M/L858R and HER2, respectively. pan-HER-IN-1 induces apoptosis and exhibits antitumor activities.

Topo I-IN-1 (Compound 14d) is a potent Topo I inhibitor. Topo I-IN-1 exhibits antitumor activity and DNA intercalative capability. Topo I-IN-1 can induce cell apoptosis.

CTX-712 is a potent inhibitor of cdc2-like kinase ( CLK ). CTX-712 inhibits inhibits cancer survival and cancer cell growth.

Orexin receptor antagonist 4 is potent and selective orexin 2 receptor (OX2R) antagonist. Orexin receptor antagonist 4 shows IC50 of 4.27 nM and 295 nM for OX2R and OX1R, respectively.

(R)-(+)-Dimethindene maleate is an orally active H 1 -receptor blocker.

AMPK activator 6 (Compound GC) activates the AMPK pathway and reduces lipid content in HepG2 and 3T3-L1 cells. AMPK activator 6 significantly suppresses the increase of total cholesterol (TC), low-density lipoprotein-C (LDL-C), triglyceride (TG), and other biochemical indices in blood serum. AMPK activator 6 has research value in non-alcoholic fatty liver disease (NAFLD) and metabolic syndrome .

Lorpucitinib (JNJ-64251330) is an orally available, selective and potent JAK kinase inhibitor for the study of inflammatory and gastrointestinal disorders associated with Janus kinase (JAK) signaling.

D4R antagonist-2 is a potent and selective D4R antagonist (IC50= 6.52 μM). D4R antagonist-2 displays favorable in vitro PK parameters and exhibits good brain penetration. D4R antagonist-2 has the research potential in Parkinson’s disease.